Fabrication Of Self Aggregatted Ropinirole Hcl Loaded Nanoparticle Using N-Acyl Chitosan Derivatives
Abstract
Self-aggregated drug delivery systems are developed through hydrophobic modification of polymers to impart amphiphilic characteristics, which promote self-assembly into nanosized carriers suitable for efficient drug delivery. N-Acyl derivative include N-Butyryl Chitosan, N-Octanoyl Chitosan, N-Lauroyl Chitosan and N-Palmitoyl Chitosan were synthesized and confirmed by FTIR and XRD. And Evaluated for Self-aggregation property and critical micellar concentration of chemically engineered chitosans and nonsubstituted chitosan was determined by pyrene fluorescence spectroscopy. Critical aggregation concentration was about 0.01 mg/ml for acylated chitosan against 1 mg/ml of chitosan. Ropinirole loaded nanoparticles of acylated chitosans and chitosan were prepared by self-assemble ultrasonication method using probe sonicator in phosphate-buffered saline (PBS) (pH 7.4). Mean ropinirole loading was higher for acylated chitosans as compared to non-substituted chitosans. The particle size of ropinirole-loaded acylated chitosan nanoparticles increased with acyl chain length due to enlargement of the hydrophobic core. Acylation reduced the positive zeta potential by decreasing free amino groups, while the low PDI (<0.5) indicated a fairly monodisperse size distribution. More sustained release of the drug from the bulkier acyl substituted chitosan was observed as compared to chitosan.
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